222 results about "Vascular permeability" patented technology

The present invention relates to development of efficacious intravitreal pharmaceutical compositions comprising a poorly water soluble agent with anti-angiogenic and/or anti vascular leakage properties in a therapeutically effective amount and a co-solvent in a suitable amount to treat or prevent diseases due to ocular neovascularization and enhanced vascular permeability. Other aspects of the invention details the development of efficacious compositions for the treatment of the said diseases via periocular, topical and oral administration.

The present invention relates to hexabasic amino amidate derivatives, their preparation process, medicines using them as active components and method for curing diseases of angiogenesis and high vascular osmolarity by using them, and also relates to the application of them as medicines.

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:

wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof.

Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided. Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.

The present invention relates to development of efficacious pharmaceutical compositions comprising a poorly water soluble active compound in a therapeutically effective amount and a co-solvent in a suitable amount to treat or prevent diseases due to ocular neovascularization and enhanced vascular permeability. In preferred aspects the composition is in the form of a gel.

The invention provides a lipidosome-polymer drug-loaded nanoparticle and a preparation method and application thereof. The lipidosome-polymer drug-loaded nanoparticle comprises a three-layer structure, wherein the innermost layer is the drug-loaded nanoparticles formed by taking an amphiphilic cationic polymer as a carrier-coated chemotherapeutic drug; the intermediate layer is a platelet inhibitor layer adsorbed onto the surface of the drug-loaded nanoparticles; and the outermost layer is a lipid bilayer connected with tumor microenvironment responsiveness polypeptides. The lipidosome-polymer drug-loaded nanoparticle disclosed by the invention is capable of specifically targeting tumor tissues, has tumor microenvironment responsiveness, and can achieve the effects of improving tumor vascular permeability without influencing functions of blood vessels at normal tissue or cell parts, enhancing permeability and retention of the drug-loaded nanoparticles to tumor cells, enhancing the EPR effect, improving enrichment of the drug-loaded nanoparticles at tumor location and realizing high tumor killing efficiency.

VEGF-D, a new member of the PDGF family of growth factors, which among other things stimulates endothelial cell proliferation and angiogenesis and increases vascular permeability, as well as nucleotide sequences encoding it, methods for producing it, antibodies and other antagonists to it, transfected or transformed host cells for expressing it, pharmaceutical compositions containing it, and uses thereof in medical and diagnostic applications.

This invention relates to the effect of Loteprednol etabonate on vascular dysfunction in the back of the eye. More specifically, this invention relates to methods of modifying a pathogenic angiogenesis in the back of an eye of a patient, the method comprising administering to a patient in need thereof a pathogenic angiogenesis modifying amount of Loteprednol etabonate. Moreover, this invention relates to methods of modifying pathologic vascular permeability manifested as retinal edema. The method compromises administering to a patient an amount of LE sufficient to reduce retinal edema.

A magnetic resonance imaging (MRI) methodology is provided for simultaneous measurement of dynamic susceptibility contrast (DSC) MRI and dynamic contrast enhanced (DCE) MRI perfusion and permeability parameters using a combination of dual echo and spiral acquisition techniques with no contrast agent preload. T1 and T2/T2* leakage effects are eliminated, thereby permitting accurate measurement of blood volume, blood flow and vascular permeability which are used in evaluating tumor angiogenesis.

The present invention provides systemic nucleic acid sequence delivery without conventional systemic administration aids (SAAs). In certain embodiments, vascular permeability agents (VPAs), such as VEGF, are used in conjunction with nucleic acid viral vectors, such as adeno-associated virus (AAV). The present invention also provides methods of treating disease by co-administration of nucleic cid sequences encoding Igf-1 and dystrophin or dystrophin-like proteins.

Compounds, compositions and methods for inhibiting vascular permeability and pathologic angiogenesis by modulating a signaling pathway delineated herein are described. Moreover, methods for producing and screening compounds and compositions capable of modulating the signaling pathway described herein, inhibiting vascular permeability, and inhibiting pathologic angiogenesis are also provided.

Modified chimeric polypeptides with improved pharmacokinetics are disclosed. Specifically, modified chimeric Flt1 receptor polypeptides that have been modified in such a way as to improve their pharmacokinetic profile are disclosed. Also disclosed are methods of making and using the modified polypeptides including but not limited to using the modified polypeptides to decrease or inhibit plasma leakage and/or vascular permeability in a mammal.

A PGD(2) receptor (DP) deficiency enhances tumor progression accompanied by abnormal vascular expansion. In tumors, angiogenic endothelial cells highly express DP receptor, and its deficiency accelerates vascular leakage and angiogenesis. Administration of a synthetic DP agonist, BW245C, markedly suppresses tumor growth as well as tumor hyperpermeability in WT mice, but not in DP-deficient mice. In a corneal angiogenesis assay and a modified Miles assay, host DP deficiency potentiates angiogenesis and vascular hyperpermeability under COX-2-active situation, whereas exogenous administration of BW245C strongly inhibits both angiogenic properties in WT mice. In an in vitro assay, BW245C does not affect endothelial migration and tube formation, processes that are necessary for angiogenesis; however, it strongly improves endothelial barrier function via an increase in intracellular cAMP production. PGD(2)/DP receptor is a newly identified regulator of tumor vascular permeability, indicating DP agonism can be exploited as a therapy for the treatment of cancer.

The present invention provides methods for the treatment and diagnosis of disorders associated with excessive vascular permeability and edema.

The invention provides a zwitterionic polymer with reductive responding antitumor activity. The zwitterionic polymer is an amphiphilic polymer formed by a disulfide bond-containing hydrophobic polycaprolactone and a hydrophilic polycarboxylic glycine betaine methacrylate. The amphiphilic polymer is self-assembled in water to form a micelle carrier of a core-shell structure, and through a physical embedding action, an antitumor drug is carried into a hydrophobic core of the nano micelle, so that the drug solubility is improved, the cycling time is prolonged, the vascular permeability synergistic effect is obtained, and the disulfide bond ruptures in a high reductive environment, so that the micelle structure is damaged so as to release adriamycin amycin, thereby further killing tumor cells; according to the polycarboxylic glycine betaine methacrylate monomer, a copolymer shows good biocompatibility, so that the toxicity of the antitumor drug is further reduced, and damage on normal tissues is reduced. An in-vitro simulative release experiment verifies that the zwitterionic polymer micelle as the drug carrier has a good release effect and is an antitumor active substance which has an application prospect.

The invention belongs to the technical field of medicine, and particularly relates to indolinone derivatives of general formula (I), deuterium of the derivatives, pharmaceutically acceptable salts of the derivatives or stereoisomer of the derivatives, wherein the indolinone derivatives serve as tyrosine kinase inhibitors, and R1, R2, R3, R4, R5, R6, R7, R8, R9, n, X and cycle A are defined as in the description. The invention further relates to preparation methods of the compounds, a pharmaceutical preparation comprising the compounds, and applications of the compounds, wherein the applications of the compounds include prevention or treatment of fibrosis diseases, treatment of excessive hyperplasia diseases, especially breast cancer, colorectal cancer and non-small cell lung cancer, anti-angiogenesis and/or reduction of vascular permeability.

The invention belongs to the technical field of medicine, and in particular relates to a tyrosine kinase inhibitor indolinone derivative as shown in formula (I), as well as a deuterium substituent, a pharmaceutically acceptable salt or a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, n and ring A are defined as in the specification. The invention further relates to a preparation method of the compounds, a pharmaceutic preparation containing the compounds as well as an application of the compounds for preparing medicines for preventing or treating fibrotic diseases and hyperplasias, in particular to breast cancer, colorectal cancer, non small cell lung cancer, anti-angiogenesis and/or reducing vascular permeability.

Disclosed herein is a modulator of vascular permeability using pulsed laser and a method for modulating vascular permeability using the same. More specifically, because the pulsed laser effectively induces vascular permeabilization, effectively delivers intravascular materials into tissues and minimizes insult to the tissues by the induced vascular permeabilization, and locally targets a subcutaneous tissue for noninvasive modulation due to its nonlinearity, it may be usefully used for modulation of permeability.

The invention relates to the technical field of biologics, in particular to a method for extracting a toxin protein which causes vascular permeability increase from white cyanea tentacles. The method comprises the following steps: unfreezing fresh white cyanea tentacles which are frozen at a super-low temperature at a low temperature, washing by a small quantity of buffer solution, collecting the buffer solution, centrifuging to obtain a supernatant and using the supernatant as cyanea crude toxin, and sequentially separating by an ion chromatographic column and a gel chromatographic column to obtain the toxin protein CnP45 which causes vascular permeability increase, wherein the molecular weight of the toxin protein is 45kD. The extracting process of the jellyfish toxin is simplified, the interference of impurity proteins is reduced, and an important method instruction is provided for the further separation and purification of jellyfish toxin ingredients.

The invention discloses a drug-loaded nanoparticle with reductive responsiveness and a preparation method and applications thereof. The structural formula of the drug-loaded nanoparticle with reductive responsiveness is as follows:, wherein x is 45, y is 15, and z is 20, or x is 45, y is 12, and z is 6. The diameter of the drug-loaded nanoparticle disclosed by the invention is 91-109 nm. PEG hydrophilic segments constitute a hydrophilic shell layer of the polymer nanoparticle, and polyphosphoesters of which a side group contains disulfide bonds constitute a hydrophobic core. The block polymer can be formed into a micelle by self-assembling in water, and then pharmaceutical molecules are loaded in the hydrophobic core of the carrier nanoparticle through a physical embedding effect, so that the drug solubility is greatly increased, the cycling time is prolonged, and the vascular permeability enhancement effect (i.e. enhanced permeability and retention EPR effect enhancement) is passively targeted to tumor tissues. The nano drug carrier can entrap various hydrophobic antineoplastic drugs such as hydrophobic drugs such as doxorubicin, paclitaxel, gefitinib, camptothecin, and the like.

Provided are methods, pharmaceutical formulations and kits thereof for the treatment and/or prevention of conditions mediated by neovascularization, abnormal angiogenesis, vascular permeability, or combinations thereof, of posterior and/or anterior tissues and fluids of the eye, including conditions associated with proliferative retinopathies, for example, diabetic retinopathy, age-related maculopathy, retinopathy of prematurity, retinopathy associated with macular edema, or retinopathy associated with sickle cell disease, using the topical administration of mecamylamine or a pharmaceutically acceptable salt thereof to the eye. Methods of preparing the pharmaceutical formulations are also provided.